Resorcin[4]arenes are not as extensively studied as their sister compounds, calix[4]arenes, owing to challenges in synthetic methodologies for their derivatization from the perceptive of molecular economy. In this tutorial review, we briefly illustrate the summary of their access methodologies together with their limitations, focusing at the derivatization of the ortho‐positions in the upper rim. We hope to spark a refreshed surge in the development of these derivatization strategies, allowing access to novel molecules and futuristic applications, putting resorcin[4]arenes at the center stage of research for which they were meant.
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